Method of producing a tablet containing a tobacco concentrate



United States Patent 3,368,567 METHOD OF PRODUCING A TABLET CON- TAININGA TOBACCO CONCENTRATE Ralph W. Speer, Memphis, Tenn., assignor to MortonPharmaceuticals, Inc., Memphis, Tenn., a corporation of Tennessee NoDrawing. Filed Mar. 23, 1965, Ser. No. 442,200

2 Claims. (Cl. 131-143) This invention relates in general to a methodfor producing a tablet incorporating a tobacco concentrate and which isintended to be located in the mouth of the user.

In View of recent medical findings, the use of tobacco, primarily in theform of cigarettes, has been considered of grave potential harm tosmokers. Since smoking is habit forming, it is most dilficult forindividuals who have enjoyed this habit over an extensive period of timeto etfectively and permanently discontinue such habit, with the resultthat many individuals, after a temporary period of abstention, resumesmoking. Various expedients have been suggested to assist smokers inWithdrawing from the smoking habit, which expedients would at leastprovide some oral satisfaction, such as, particularly, chewing gum.However, such expedients have not proved satisfying and many smokerswill merely place an unlighted cigarette in their mouth to obtain atobacco taste which might also be obtained through chewing tobacco.However, the former, obviously, does not provide the desired tastesensation, much less physiological reaction associated with smoking andthe latter is not consonant with most business and social situations.

Therefore, it is an object of the present invention to provide,preferably in tablet form, a tobacco concentrate preparation which isfor buccal and sublingual usage; which preparation contains nicotine andother tobacco alkaloids in soluble form so that the user may obtaintherefrom a physiological response associated with smok- 1ng.

Another object of the present invention is to provide a tobaccoconcentrate preparation which is devoid of some of the various resinsand tars formed during the combustion of the leaf tobacco and which aredeemed to contain the agents harmful to smokers so that the use of thesaid preparation does not involve some of the risks encountered insmoking.

A still further object of the present invention is to provide a tobaccoconcentrate preparation for oral usage and which contains a true tobaccoflavor but without the pungency and acridity encountered in tobaccosmoke.

It is an additional object of the present invention to provide a methodfor producing a tobacco concentrate which is amenable to economic, highvolume production with quality maintenance.

With the above noted objects, my invention resides in the novel methodpresently described in the following specification and pointed out inthe claims.

In essence, the present invention contemplates the production of atabletized tobacco concentrate preparation containing the activeingredients of tobacco, primarily the alkaloidal material which containsnicotine, and an edible carrier, such a dextrose, sucrose, lactose, orthe like with the carrier constituting the major portion by weight ofthe tablet. The method for producing such preparation fundamentallycomprises the subjection of ground leaf tobacco to a solubilizing agentfor forming water-soluble salts of the alkaloids, separating the samefrom the residue containing tar producing materials, resins, and thelike material, then impregnating the carrier material in granulated formwith the alkaloid salts for tabletizing subsequent to driving action.

3,368,567 Patented Feb. 13, 1968 The physiological active ingredients oftobacco are thought to consist of alkaloids which may range from 2percent to 8 percent of the whole tobacco. However, generally in thetobacco normally used for cigarette production, the content is about 4percent. Nicotine constitutes one of the primary components of thealkaloidal group. The remainder of the tobacco consists of amultiplicity of organic components which do not materially conduce tothe above mentioned physiological response obtained by the smoker. Suchother materials do comprehend ingredients which have been considered aspotentially extremely harmful agents to humans, such as particularly thetar producing materials and resins. In the present invention thealkaloids are extracted from the Whole tobacco, that is, separated fromthe other agents and are then applied to a suitable vehicle for humanusage to provide the user with both the physiological reaction as wellas the taste of tobacco. As will be developed more fully hereinbelow,the preparation of this invention embodies varying concentrations of theextract, alkaloidal, material so that a desired strength of tobacco maybe presented. It has been found that some individuals are quitesensitive to tobacco alkaloids and a relatively small amount issufficient to promote a particular re sponse; whereas, others cantolerate greater concentrations. The present invention is adapted forproduction to accommodate the multiplicity of choice of tobaccostrength.

It has been established that tablets, lozenges, and the like formed inaccordance with this invention do not cause staining of the teeth orgums, nor cause the imparting of breath odors, while the taste is of asubstantially pure tobacco character, being devoid of the pungency andacridity encountered in tobacco smoking. The tobacco cencentrate tabletsare preferably used sublingually being allowed to dissolve slowly in themouth for absorption by the mucous membranes for entry into the bloodstream to bring about the customary response. It is, of course, apparentthat such tablets may be chewed, but by doing so the particular responsemay be lost.

Tablets produced in accordance with this invention may be of anysuitable size and weight, but it has been found that a weight of about650 milligrams is preferable, corresponding to a generally acceptedtablet size and contain between to 99 /2 percent by weight of an inert,edible filler, or excipient base which may be of any well-known materialsuch as the sugars, i.e., dextrose, sucrose, and lactose; salts, i.e.,sodium chloride, potassium chloride, magnesium sulphate; and starches,and cellulose bases such as methyl cellulose, carboxy methyl cellulose,etc.; the other ingredient, being the active principles in tobacco,namely, the alkaloids in water soluble form, constituting between onehalf and 10 percent by weight, of the tablet. It will be observedhereinbelow that the relationship of filler to active tobacco principleswill be determined by choice, as the relative concentration of thealkaloids will be dictated by the desired strength.

It has been determined that a content of less than one half percent byweight of the alkaloids provides a substantially undetectablephysiological response, while a content greater than 10 percent byweight has proved to be of such strength as to be unacceptable. In orderto prepare tablets of the type hereinabove described, a quan- 'ty ofleaf tobacco, which, for purposes of illustration only, may be in theamount of 55 pounds, is subjected to the customary tobacco dryingprocedure, and is then ground or comminuted into fine particlesapproximating a dust to present maximum surface for the ensuingextraction procedure. The ground tobacco is then steeped in watersufficient for extraction of the alkaloids. With 55 pounds of tobacco,it has been discovered that 10 gallons of water is adequate for this.The water conduces to the solubilizing of the alkaloids and to promotethe extraction. Concentrated mineral acid is added such as sulphuricacid which, with 55 pounds of tobacco, may be approximately one pound.The acid reacts with the alkaloids which are basic in character to formcomplex watersoluble sulphates for separation from the whole tobacco. Topromote the extraction process, the water is subjected to high speedagitation, while the finely ground tobacco is blended thereinto, withthe agitation being continued as the mineral acid is added. Subsequentto the addition of the acid, the mixture is heated to a temperature ofbetween 190 degrees to 200 degrees F. for a period of about eight hours.The heat and the agitation considerably accelerate the process forforming the desired water soluble alkaloidal salts. Upon termination ofthe heating operation, the mixture resembles a slurry which is allowedto cool and settle for a limited period of time, such as overnight. Thenthe cooled, slurry is pressure filtered for withdrawal of the motherliquor which contains the alkaloidal salts; the residue being comprisedof the tars, resins, other aniline materials, as well as cellulosiccompounds, fibrous matter, and the like. To the filtrate is addedsuflicient alkali to neutralize any excess mineral acid. Ammonia,caustic soda, potassium hydroxide, magnesium hydroxide and similarinorganic bases may be utilized for forming salts with the excesssulphuric acid, as in this case. The addition of the alkali will tend toadjust the pH of the mixture to substantial neutrality as between 6 and8. The mixture will contain the alkaloids either in the form of solublesalts or in natural form, depending upon the degree of neutralization ofthe extract.

The filtrate, which contains the now water soluble alkaloids is appliedupon granulated, edible excipient bases presented, as on trays, forabsorption thereby. The excipient bases are of any suitable, inertmaterial such as sugars, i.e., dextrose, sucrose, and lactose; salts,i.e., sodium chloride, potassium chloride, magnesium sulphate; andstarches, and cellulose bases such as methyl cellulose, carboxy methylcellulose, etc., cellulose base materials, gums such as gum arabic, andother well-known vehicles of this type. The granulated vehicularmaterials with the applied filtrate is then allowed to dry at arelatively low heat not to exceed 110 degrees P. so that the dryingprocess is gradually but thoroughly accomplished without any undesiredcharring or heat degradation of the materials. The amount of excipientbase provided for receiving the filtrate will be determined by theintended proportion of such base in the ultimate tablet. Generallyspeaking, the quantity of base will be in the nature of 300 to 400pounds for the initial 55 pounds of tobacco; but with the reservationthat such amount will be related to the concen tration of the alkaloidsalts.

Subsequent to drying, a conventional lubricant is applied to the mixtureof the excipient bases and the alkaloid salts, and then the mass iscompressed into tablet form in accordance with recognized tabletingtechniques.

It is understood that, if desired, additional flavoring may be supplied,such as menthol, mint, licorice, etc.

The tablets or lozenges as thus formed are ready for human usage and, asindicated above, are free of some of the disadvantages encountered whensmoking yet capable of supplying the tobacco craving of individuals whoprefer to discontinue smoking.

It should be evident from the foregoing that mineral acids, other thansulphuric, are adapted for the alkaloid extraction process, such ashydrochloric, as well as various organic acids, among which may beacetic, lactic and the like. In practice, sulphuric acid has proved tobe highly efficient. Additionally, the extraction process may beeffected in a water-alcohol phase rather than merely a water phase, withthe proportion ranging up to equal amounts of water and alcohol. Thelower molecular alcohols have proved quite effective in this connection.

in order to hasten the extraction process, the same may be brought aboutin a closed system under pressure, or

additional heat may be used with an open vessel. It is even possible toeffect extraction by subjecting the mixture to agitation alone underatmospheric conditions, but it will be appreciated that such a processis indeed lengthy and not conducive to high volume, high speedproduction. The desired conditions for extraction are those which willpromote same most rapidly and most thoroughly, and the conditionshereinabove set forth in the example have been of demonstrated efficacy.

As mentioned hereinabove, the alkaloid content of leaf tobacco isnormally in the range of about 2 percent to 8 percent, with 4 percentbeing the most widely encountered. Generally speaking, the nicotiniccontent is considered coextensive with the alkaloid content. After themother liquor has been separated from the slurry mixture, it ispreferable to assay same to determine the nicotine or alkaloid contentin order to evaluate the extent of the extract. The nicotine alkaloidcontent of the extract is chemically evaluated and compared, with thatof the starting tobacco. Sufiicient quantity of the extract is used tomake a finished tablet having a nicotine alkaloid content to beequivalent to not less than 10 percent and not more than 70 percent ofwhole tobacco equivalent. For example, if the analysis of the extract ofa tobacco having nicotine content of 4 percent demonstrates aconcentration of nicotine of 2 percent, that is 2 pounds of nicotine per100 pounds of extract, and it was desired to have the resulting tabletsincorporate a whole tobacco equivalent of 20 percent, 40 pounds of theextract would be applied to the vehicle so that for each 99.2 pounds ofvehicle, .8 pound of nicotine would be mixed therewith to make 100pounds. Accordingly, if a single tablet has a weight of 650 milligrams,and the whole tobacco equivalent was 20 percent, then the nicotinecontent of the tablet would approximate S milligrams per tablet. Thisamount would compare favorably with the customary 3 /2 milligrams ofnicotine in the average cigarette. In accordance with the foregoing, itis apparent that the nicotine content of the finished tablet may beeasily adjusted in accordance with laboratory practice to provide thedesired strength.

In view of the foregoing, a range of between 1 milligram andapproximately 15 milligrams of nicotine can be easily incorporated in atablet and set the preferred limits for normal usage.

Additionally, another factor to be considered is the amount of ediblefiller to be used within a given concentration of the active principlesof tobacco or alkaloids. It has been found that in the tablet of thepresent invention there should be no less than percent by weight offiller and with the upper limit being 99.50 percent by weight thereof.Correspondingly, the tobacco concentrate or alkaloid content would rangefrom a low of .50 percent to 10 percent.

In view of the foregoing, it will be seen that the present inventionprovides a tabletized tobacco concentrate which may be produced in aneconomic manner designed for high volume production, involving anextraction and a concentration with an acid medium and which allows forproducing tablets of desired whole tobacco equivalent so that individualtastes may be accommodated.

The disclosed preparation, it is believed, avoids the dangers believedto be encountered during the inhalation of smoke resulting from thechemical degradation of whole natural tobacco. The incorporatedconcentrated alkaloids provide the desired physiological responsewithout the necessity of the said smoke inhalation.

It should be understood that changes in the methods, compositions,percentages, and combinations set forth may be made without departingfrom the nature and principle of my invention.

Having thus described my invention, what I claim and desire to secure byLetters Patent is:

1. A. method of producing a tobacco concentrate comprising providingfinely comminuted dried leaf tobacco, subjecting the dried tobacco to anaqueous phase and to an absorbent, inert, edible base, to the extentthat it constitutes less than 10% of the said base, permitting theliquid to dry, and then compressing the resultant material into tabletform.

2. A method of producing a tobacco concentrate which comprises providinga finely ground, dry leaf tobacco, subjecting the dried tobacco toalcohol-aqueous phase and concentrated mineral acid, subjecting themixture to agitation and heat within the range of 190 degrees F. to 200degrees F. for a period of approximately 8 hours, neutralizing theexcess acid in the mixture, subjecting the mixture to pressurefiltering, applying the filtrate to an absorbent, inert, edible base, tothe extent that it constitutes less than 10% of the said base,permitting the mixture of the filtrate and base to dry, adding lubricantto such mixture and then compressing the said filtrate, base andlubricant into tablet form.

References Cited UNITED STATES PATENTS 639,365 12/1899 Dudley 1311790,138 5/1905 Koelliker 131-143 X 802,487 10/1905 Wimmer 131-1432,576,021 11/1951 Koree 131-2 2,033,495 3/1936 Taylor et al. 167-533,067,068 12/1962 Finberg 131-2 3,120,233 2/1964 Battista et al. 131-143X 3,145,717 8/1964 Osborne et al. 131-143 X 3,166,078 1/1965 Parmele etal. 131-5 3,255,760 6/1966 Selke 1318 SAMUEL KOREN, Primary Examiner.

MELVIN D. REIN, Examiner.

1. A METHOD OF PRODUCING A TOBACCO CONCENTRATE COMPRISING PROVIDINGFINELY COMMINUTED DRIED LEAF TOBACCO, SUBJECTING THE DRIED TOBACCO TO ANAQUEOUS PHASE AND CONCENTRATED MINERAL ACID, SUBJECTING THE MIXTURE TOAGITATION, NEUTRALIZING THE EXCESS ACID IN THE MIXTURE, WITHDRAWING THELIQUID FROM THE MIXTURE, APPLYING THE LIQUID TO AN ABSORBENT, INERT,EDIBLE BASE, TO THE EXTENT THAT IT CONSTITUTES LESS THAN 10% OF THE SAIDBASE, PERMITTING THE LIQUID TO DRY, AND THEN COMPRESSING THE RESULTANTMATERIAL INTO TABLET FORM.